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Bioorg Med Chem Lett. 2008 Jan 15;18(2):755-8. Epub 2007 Nov 17.

Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template.

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  • 1Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.


In our effort to find potent, orally bioavailable CGRP receptor antagonists for the treatment of migraine, a novel series based on a pyridinone template was investigated. After optimizing the privileged structure and the placement of the attached phenyl ring, systematic SAR was carried out on both the N-alkyl and C-5 aryl substituents. Several analogs with good potency and pharmacokinetic profiles were identified.

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